Modulation of insulin-like growth factor-1 receptor and its signaling network for the treatment of cancer: Current status and future perspectives

Oncology Reviews

Volumn 7, Issue 1, 2013, Pages 12-26

  Jin, Meizhong ^a   Buck, Elizabeth ^a   Mulvihill, Mark J ^a  

^a OSI PHARMACEUTICALS INC   (United States)

Author keywords

Cancer; Drug combination; Inhibitor; Insulin receptor; Insulin like growth factor 1 receptor

Indexed keywords

1 [4 [(5 CYCLOPROPYL 1H PYRAZOL 3 YL)AMINO]PYRROLO[2,1 F][1,2,4]TRIAZIN 2 YL] N (6 FLUORO 3 PYRIDINYL) 2 METHYL 2 PYRROLIDINECARBOXAMIDE; ANTINEOPLASTIC AGENT; ARRY 438162; AXL 1717; BMS 536924; BMS 695735; CARBOPLATIN; CETUXIMAB; CIXUTUMUMAB; DALOTUZUMAB; DOCETAXEL; DOXORUBICIN; DUSIGITUMAB; ERLOTINIB; EVEROLIMUS; FIGITUMUMAB; GANITUMAB; GEMCITABINE; GSK 1838705A; GSK 1904529A; LINSITINIB; PACLITAXEL; PANITUMUMAB; PEMETREXED; PICROPODOPHYLLIN; R 1507; RIDAFOROLIMUS; ROBATUMUMAB; SORAFENIB; TEMOZOLOMIDE; TEMSIROLIMUS; TRASTUZUMAB; UNCLASSIFIED DRUG; UNINDEXED DRUG; VEMURAFENIB; XL 228;

ADVANCED CANCER; ANTIPROLIFERATIVE ACTIVITY; BREAST CANCER; BREAST METASTASIS; CANCER THERAPY; CELL PROLIFERATION; CELL SURVIVAL; DRUG BIOAVAILABILITY; DRUG EFFICACY; ESTROGEN RECEPTOR POSITIVE BREAST CANCER; EWING SARCOMA; HEAD AND NECK CANCER; HEAD AND NECK SQUAMOUS CELL CARCINOMA; HUMAN; LARGE CELL NEUROENDOCRINE CARCINOMA; LIVER CELL CARCINOMA; LUNG ADENOCARCINOMA; LUNG NON SMALL CELL CANCER; LUNG SQUAMOUS CELL CARCINOMA; METASTATIC COLORECTAL CANCER; MULTIPLE MYELOMA; NEUROECTODERM TUMOR; OSTEOSARCOMA; OVARY CANCER; OVARY CARCINOMA; PRIORITY JOURNAL; PROSTATE CANCER; REVIEW; RHABDOMYOSARCOMA; SARCOMA; SKIN CARCINOMA; SOFT TISSUE SARCOMA; SOLID TUMOR; SYNOVIAL SARCOMA;

EID: 84878632366     PISSN: 19705557     EISSN: 19705565     Source Type: Journal    
DOI: 10.4081/oncol.2013.e3     Document Type: Review

References (81)

1. Myal Y, Shiu R P, Bhaumick B, et al. Receptor binding and growth-promoting activity of insulin-like growth factors in human breast cancer cells (T-47D) in culture. Cancer Res 1984; 44: 5486-90.
2. Pollak MN, Perdue JF, Margolese RG, et al. Presence of somatomedin receptors on primary human breast and colon carcinomas. Cancer Lett 1987; 38: 223-30.
3. Sell C, Rubini M, Rubin R, et al. Simian virus 40 large tumor antigen is unable to transform mouse embryonic fibroblasts lacking type 1 insulin-like growth factor receptor. Proc Natl Acad Sci U S A 1993; 90: 11217-21.
4. Rubin R, Baserga R. Insulin-like growth factor-I receptor. Its role in cell proliferation, apoptosis, and tumorigenicity. Lab Invest 1995; 73: 311-31.
5. Kondo M, Suzuki H, Ueda R, et al. Frequent loss of imprinting of the H19 gene is often associated with its overexpression in human lung cancers. Oncogene 1995; 10: 1193-8.
6. Kaiser U, Schardt C, Brandscheidt D, et al. Expression of insulinlike growth factor receptors I and II in normal human lung and in lung cancer. J Cancer Res Clin Oncol 1993; 119: 665-8.
7. Ma J, Giovannucci E, Pollak M, et al. A prospective study of plasma C-peptide and colorectal cancer risk in men. J Natl Cancer Inst 2004; 96: 546-53.
8. LeRoith D, Roberts CT Jr. The insulin-like growth factor system and cancer. Cancer Lett 2003; 195: 127-37.
9. Ceresa B P, Pessin JE. Insulin regulation of the Ras activation/ inactivation cycle. Mol Cell Biochem 1998; 182: 23-9.
10. Gooch JL, Van Den Berg CL, Yee D. Insulin-like growth factor (IGF)-I rescues breast cancer cells from chemotherapy-induced cell death-proliferative and anti-apoptotic effects. Breast Cancer Res Treat 1999; 56: 1-10.
11. Turner BC, Haffty BG, Narayanan L, et al. Insulin-like growth factor-I receptor overexpression mediates cellular radioresistance and local breast cancer recurrence after lumpectomy and radiation. Cancer Res 1997; 57: 3079-83.
12. Jerome L, Alami N, Belanger S, et al. Recombinant human insulinlike growth factor binding protein 3 inhibits growth of human epidermal growth factor receptor-2-overexpressing breast tumors and potentiates herceptin activity in vivo. Cancer Res 2006; 66: 7245-52
13. Wittman M, Velaparthi U, Vyas D. Recent progress in the development of small molecule inhibitors of insulin-like growth factor-I receptor kinase. Annu Rep Med Chem 2009; 44: 281-99.
14. Li R, Pourpak A, Morris SW. Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach. J Med Chem 2009; 52: 4981-5004.
15. Jin M, Wang J, Buck E, Mulvihill MJ. Small-molecule ATP-competitive dual IGF-1R and insulin receptor inhibitors: structural insights, chemical diversity and molecular evolution. Future Med Chem 2012; 4: 315-28.
16. Karp DD, Paz-Ares LG, Novello S, et al. Phase II study of the antiinsulin-like growth factor type 1 receptor antibody CP-751,871 in combination with paclitaxel and carboplatin in previously untreated, locally advanced, or metastatic non-small-cell lung cancer. J Clin Oncol 2009; 27: 2516-22.
17. Haluska P, Shaw H, Batzel GN, et al. Phase I dose escalation study of the anti-IGF-1R monoclonal antibody CP-751,871 in patients with refractory solid tumors. ASCO Annual Meeting Abstracts 2007; 25: 3586.
18. Jassem J, Langer CJ, Karp DD, et al. Randomized, open label, phase III trial of figitumumab in combination with paclitaxel, carboplatin versus paclitaxel, carboplatin in patients with non-small cell lung cancer (NSCLC). J Clin Oncol 2010; 28: 7500.
19. García-Echeverría C, Pearson MA, Marti A, et al. In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell 2004; 5: 231-9.
20. Isebaert SF, Swinnen JV, McBride WH, Haustermans KM. Insulinlike growth factor-type 1 receptor inhibitor NVP-AEW541 enhances radiosensitivity of PTEN wild-type but not PTEN-deficient human prostate cancer cells. Int J Radiat Oncol Biol Phys 2011; 1: 239-47.
21. Warshamana-Greene GS, Litz J, Buchdunger E, et al. The insulinlike growth factor-I receptor kinase inhibitor, NVP-ADW742, sensitizes small cell lung cancer cell lines to the effects of chemotherapy. Clin Cancer Res 2005; 11: 1563-71.
22. Fagan DH, Uselman RR, Sachdev D, Yee D. Acquired resistance to tamoxifen is associated with loss of the type I insulin-like growth factor receptor: implications for breast cancer treatment. Cancer Res 2012; 72: 3372-80.
23. Ji Q, Mulvihill MJ, Rosenfeld-Franklin M, et al. A novel, potent, and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor dependent tumor growth in vivo. Mol Cancer Ther 2007; 6: 2158-67.
24. Girnita A, Girnita L, Del PF, et al. Cyclolignans as inhibitors of the insulin-like growth factor-1 receptor and malignant cell growth. Cancer Res 2004; 64: 236-42.
25. Menu E, Jernberg-Wiklund H, Stromberg T, et al. Inhibiting the IGF-1 receptor tyrosine kinase with the cyclolignan PPP: an in vitro and in vivo study in the 5T33MM mouse model. Blood 2006; 107: 655-60.
26. Karasic TB, Hei TK, Ivanov VN. Disruption of IGF-1R signaling increases TRAIL-induced apoptosis: A new potential therapy for the treatment of melanoma. Exp Cell Res 2010; 316: 1994-2007.
27. Duan Z, Choy E, Harmon D, et al. Insulin-like growth factor-I receptor tyrosine kinase inhibitor cyclolignan picropodophyllin inhibits proliferation and induces apoptosis in multidrug resistant osteosarcoma cell lines. Mol Cancer Ther 2009; 8: 2122-30.
28. Linder S, Shoshan MC, Gupta RS. Picropodophyllotoxin or podophyllotoxin does not induce cell death via insulin-like growth factor-I receptor. Cancer Res 2007; 67: 2899-900.
29. Morphy R. Selectively nonselective kinase inhibition: striking the right balance. J Med Chem 2010; 53: 1413-37.
30. Buck E, Mulvihill M. Small molecule inhibitors of the IGF-1R/IR axis for the treatment of cancer. Expert Opin Investig Drugs 2011; 20: 605-21.
31. Carapancea M, Cosaceanu D, Budiu R, et al. Dual targeting of IGF-1R and PDGFR inhibits proliferation in high-grade gliomas cells and induces radiosensitivity in JNK-1 expressing cells. J Neurooncol 2007; 85: 245-54.
32. Rozengurt E, Sinnett-Smith J, Kisfalvi K. Crosstalk between insulin/insulin-like growth factor-1 receptors and G protein coupled receptor signaling systems: a novel target for the antidiabetic drug metformin in pancreatic cancer. Clin Cancer Res 2010; 16: 2505-11.
33. Giorgino F, Belfiore A, Milazzo G, et al. Overexpression of insulin receptors in fibroblast and ovary cells induces a ligand-mediated transformed phenotype. Mol Endocrinol 1991; 5: 452-9.
34. Buck E, Gokhal PC, Koujak S, et al. Compensatory insulin receptor (IR) activation on inhibition of insulin-like growth factor-1 receptor (IGF-1R): rationale for cotargeting IGF-1R and IR in cancer. Mol Cancer Ther 2010; 9: 2652-64.
35. Heuson JC, Legros N. Effect of insulin and of alloxan diabetes on growth of the rat mammary carcinoma in vivo. Eur J Cancer 1970; 6: 349-51.
36. Heuson JC, Legros N. Influence of insulin deprivation on growth of the 7, 12-dimethylbenz(a)anthracene-induced mammary carcinoma in rats subjected to alloxan diabetes and food restriction. Cancer Res 1972; 32: 226-32.
37. Sciacca L, Costantino A, Pandini G, et al. Insulin receptor activation by IGF-II in breast cancers: evidence for a new autocrine/paracrine mechanism. Oncogene 1999; 18: 2471-9.
38. Vella V, Pandini G, Sciacca L, et al. A novel autocrine loop involving IGF-II and the insulin receptor isoform-A stimulates growth of thyroid cancer. J Clin Endocrinol Metab 2002; 87: 245-54.
39. Sciacca L, Prisco M, Wu A, et al. Signaling differences from the A and B isoforms of the insulin receptor (IR) in 32D cells in the presence or absence of IR substrate-1. Endocrinology 2003; 144: 2650-8.
40. Cox ME, Gleave ME, Zakikhani M, et al. Insulin receptor expression by human prostate cancers. Prostate 2009; 69: 33-40.
41. Pollak M. Insulin and insulin-like growth factor signaling in neo-plasia. Nat Rev Cancer 2008; 8: 915-28.
42. Pollak M. Targeting insulin and insulin-like growth factor signaling in oncology. Curr Opin Pharmacol 2008; 8: 384-92.
43. Fulzele K, DiGirolamo DJ, Liu Z, et al. Disruption of the insulin-like growth factor type 1 receptor in osteoblasts enhances insulin signaling and action. J Bio Chem 2007; 282: 25649-58.
44. Entingh-Pearsall A, Kahn CR. Differential roles of the insulin and insulin-like growth factor-I (IGF-I) receptors in response to insulin and IGF-I. J Biol Chem 2004; 279: 38016-24.
45. Mulvihill MJ, Ji Q, Coate H, et al. Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors. Bioorg Med Chem 2008; 16: 1359-75
46. Mulvihill MJ, Cooke A, Rosenfeld-Franklin M, et al. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future Med Chem 2009; 1: 1153-71.
47. Lindsay CR, Chan E, Evans TR, et al. Phase I dose escalation study of the continuous oral dosing of OSI-906, an insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase inhibitor, in patients with advanced solid tumors. J Clin Oncol 2009; 27: Abstract 2559.
48. Mulvihill MJ. OSI-906, a selective, orally available dual inhibitor of IGF-1R and IR currently undergoing clinical testing in a phase III clinical trial in ACC patients. ACS National Meeting Abstracts 2010; MEDI-8.
49. Wittman MD, Carboni JM, Yang Z, et al. Discovery of a 2,4-disubstituted pyrrolo-[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development. J Med Chem 2009; 52: 7360-3.
50. Buchanan JL, Newcomb JR, Carney D P, et al. Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors. Bioorg Med Chem Lett 2011; 21: 2394-9.
51. Ducray R, Simpson I, Jung FH, et al. Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase. Bioorg Med Chem Lett 2011; 21: 4698-701.
52. Ducray R, Jones CD, Jung FH, et al. Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline. Bioorg Med Chem Lett 2011; 21: 4702-4.
53. Seshacharyulu P, Ponnusamy M P, Haridas D, et al. Targeting the EGFR signaling pathway in cancer therapy. Expert Opin Ther Target 2012; 16: 15-31.
54. Ludovini V, Bellezza G, Pistola L, et al. High coexpression of both insulin-like growth factor receptor-1 (IGFR-1) and epidermal growth factor receptor (EGFR) is associated with shorter disease-free survival in resected non-small-cell lung cancer patients. Ann Oncol 2009; 20: 842-9.
55. Desbois-Mouthon C, Cacheux W, Blivet-Van Eggelpoël MJ, et al. Impact of IGF-1R/EGFR cross-talks on hepatoma cell sensitivity to gefitinib. Int J Cancer 2006; 119: 2557-66.
56. Hu Y P, Patil SB, Panasiewicz M, et al. Heterogeneity of receptor function in colon carcinoma cells determined by cross-talk between type I insulin-like growth factor receptor and epidermal growth factor receptor. Cancer Res 2008; 68: 8004-13.
57. Ueda S, Hatsuse K, Tsuda H, et al. Potential crosstalk between insulin-like growth factor receptor type 1 and epidermal growth factor receptor in progression and metastasis of pancreatic cancer. Mod Pathol 2006; 19: 788-96.
58. Riedemann J, Takiguchi M, Sohail M, et al. The EGF receptor interacts with the type 1 IGF receptor and regulates its stability. Biochem Biophys Res Commun 2007; 13: 707-14.
59. Denley A, Cosgrove LJ, Booker GW, et al. Molecular interactions of the IGF system. Cytokine Growth Factor Rev 2005; 16: 421-39.
60. Goetsch L, Gonzalez A, Leger O, et al. Combination of IGF-IR and EGFR antibodies. Int J Cancer 2005; 113: 316-28.
61. Wilsbacher JL, Zhang Q, Tucker LA, et al. Combinations of gefitinib and NVP-ADW742 caused synergistic decreases in cellular proliferation across a diverse set of cancer cell lines. J Biol Chem 2008; 283: 23721-30.
62. Buck E, Eyzaguirre A, Rosenfeld-Franklin M, et al. Feedback mechanisms promote cooperativity for small molecule inhibitors of epidermal and insulin-like growth factor receptors. Cancer Res 2008; 68: 8322-32.
63. Hubbard RD, Bamaung NY, Fidanze SD, et al. Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases. Bioorg Med Chem Lett 2009; 19: 1718-21.
64. Wang GT, Mantei RA, Hubbard RD, et al. Substituted 4-amino-1H-pyrazolo[3, 4-d]pyrimidines as multi-targeted inhibitors of insulinlike growth factor-1 receptor (IGF1R) and members of the ErbB-family receptor kinases. Bioorg Med Chem Lett 2010; 19: 6067-71.
65. Fidanze SD, Erickson SA, Wang GT, et al. Imidazo[2,1-b]thiazoles: Multi-targeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor kinases. Bioorg Med Chem Lett 2010; 20: 2452-5.
66. Tandon R, Kapoor S, Vali S, et al. Dual epidermal growth factor receptor (EGFR)/insulin-like growth factor-1 receptor (IGF-1R) inhibitor: a novel approach for overcoming resistance in anticancer treatment. Eur J Pharm 2011; 67: 56-65.
67. O'Reilly KE, Rojo F, She QB, et al. mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res 2006; 66: 1500-8.
68. Zhang T, Feldman I, Sathyanarayanan S, et al. Preclinical and molecular profiling data suggest LumB breast cancer as a potential indication for co-targeting IGF1R and mTOR with MK-0646 and MK-8669. Clin Cancer Res 2010; 16: PR3.
69. Shaw RJ, Bardeesy N, Manning BD, et al. The LKB1 tumor suppressor negatively regulates mTOR signaling. Cancer Cell 2004; 6: 91-9.
70. Byers LA, Cortez MA, Yang C, et al. Proteomic profiling of signaling pathways in LKB1 deficient non-small cell lung cancers (NSCLC) identifies novel therapeutic targets including IGF1R pathway. AACR Annual Meeting Abstracts 2013; 2403.
71. Zask, A, Verheijen, JC, Richard, DJ. Recent advances in the discovery of small-molecule ATP competitive mTOR inhibitors: a patent review. Expert Opin Ther Pat 2011; 21: 1109-27.
72. Villanueva J, Vultur A, Lee JT, et al. Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by co-targeting MEK and IGF-1R/PI3K. Cancer Cell 2010; 18: 683-95.
73. Aplin AE, Kaplan FM, Shao Y. Mechanisms of resistance to RAF inhibitors in melanoma. J Invest Dermatol 2011; 131: 1817-20.
74. Smith DC, Britten CD, Clary DO, et al. A phase 1 study of XL228, a potent IGF-1R / AURORA / SRC inhibitor. J Clin Oncol 2009; 27: Abstract 3512.
75. Blecha JE, Anderson MO, Chow JM, et al. Inhibition of IGF-1R and lipoxygenase by nordihydroguaiaretic acid (NDGA) analogs. Bioorg Med Chem Lett 2007; 17: 4026-9.
76. Friedlander TW, Weinberg VK, Huang Y, et al. A phase II study of insulin-like growth factor receptor inhibition with nordihydroguaiaretic acid in men with non-metastatic hormone-sensitive prostate cancer. Oncol Rep 2012; 27: 3-9.
77. Meyer AN, McAndrew CW, Donoghue DJ. Nordihydroguaiaretic acid inhibits an activated fibroblast growth factor receptor 3 mutant and blocks downstream signaling in multiple myeloma cells. Cancer Res 2008; 68: 7362-70.
78. Arteaga CL, Kitten LJ, Coronado EB, et al. Blockade of the type I somatomedin receptor inhibits growth of human breast cancer cells in athymic mice. J Clin Invest 1989; 84: 1418-23.
79. Bartella V, De Marco P, Malaguarnera R, et al. New advances on the functional cross-talk between insulin-like growth factor-I and estrogen signaling in cancer. Cell Signal 2012; 24: 1515-21.
80. Apse B, Blair JA, Gonzalez B, et al. Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Bio 2008; 4: 691-9.
81. Knight ZA, Lin H, Shokat KM. Targeting the cancer kinome through polypharmacology. Nat Rev Cancer 2010; 10: 130-7.